Radiopharmaceutical chemistry for positron emission tomography.

Abstract:

:Molecular imaging is an emerging technology that allows the visualization of interactions between molecular probes and biological targets. Molecules that either direct or are subject to homeostatic controls in biological systems could be labeled with the appropriate radioisotopes for the quantitative measurement of selected molecular interactions during normal tissue homeostasis and again after perturbations of the normal state. In particular, positron emission tomography (PET) offers picomolar sensitivity and is a fully translational technique that requires specific probes radiolabeled with a usually short-lived positron-emitting radionuclide. PET has provided the capability of measuring biological processes at the molecular and metabolic levels in vivo by the detection of the gamma rays formed as a result of the annihilation of the positrons emitted. Despite the great wealth of information that such probes can provide, the potential of PET strongly depends on the availability of suitable PET radiotracers. However, the development of new imaging probes for PET is far from trivial and radiochemistry is a major limiting factor for the field of PET. In this review, we provided an overview of the most common chemical approaches for the synthesis of PET-labeled molecules and highlighted the most recent developments and trends. The discussed PET radionuclides include ¹¹C (t₁(/)₂=20.4min), ¹³N (t₁(/)₂=9.9min), ¹⁵O (t₁(/)₂=2min), ⁶⁸Ga (t₁(/)₂=68min), ¹⁸F (t₁(/)₂=109.8min), ⁶⁴Cu (t₁(/)₂=12.7h), and ¹²⁴I (t₁(/)₂=4.12d).

journal_name

Adv Drug Deliv Rev

authors

Li Z,Conti PS

doi

10.1016/j.addr.2010.09.007

subject

Has Abstract

pub_date

2010-08-30 00:00:00

pages

1031-51

issue

11

eissn

0169-409X

issn

1872-8294

pii

S0169-409X(10)00185-7

journal_volume

62

pub_type

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